# US 4,397,863 A · Inhibition of respiratory syncytial virus-induced cell fusion by amidino compounds

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- Number: US 4,397,863 A
- Document ID: US4397863A
- Status: Granted
- Kind: A
- Application number: 06/366,652
- Filed: 1982-04-08
- Granted: 1983-08-09
- Earliest claimed: 1980-08-26
- Assignees: Research Triangle Institute
- Inventors: Richard R. Tidwell; Edward J. Dubovi; Joachim D. Geratz
- Web page: https://patentgrep.com/patent/US4397863A

## CPC

- A61K 31/40: having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K 31/155: Amidines ([IMAGE cpc-sch-A61K-1029.gif]), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
- A61K 31/34: having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
- A61K 31/415: 1,2-Diazoles
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)

## Abstract

A number of aromatic mono- and bis-amidines are capable of blocking cell fusion induced by Respiratory Syncytial (RS) virus. Suitable amidino compounds include those selected from the group consisting of 1-4-di(4-amidinophenoxy)-2-butanol; bis(5-amidino-2-benzimidazolyl)methane; 1,2-bis(5-amidino-2-benzimidazolyl )ethane; 5-amidino-indole; 5-amidinobenzimidazole, 5-amidino-1-methylindole and 5-amidino-1-(4-amidinobenzyl)indole. The most powerful of the compounds, bis(5-amidino-2-benzimidazolyl)methane (BABIM), is able to achieve complete suppression of syncytium formation at a concentration of 1 .mu.M. Inhibition occurs in RS virus-infected Hep-2 cells as well as CV-1 cells. BABIM also causes a significant retardation of RS virus penetration, but does not interfere with adsorption. Addition of the amidines after the penetration of RS virus does not affect single cycle yields. The compounds may be used in the prophylactic control of RS virus in man.

## Claims

### Claim 1

A method for the treatment of respiratory syncytial virus-induced cell fusion which comprises administering to a host in need of said treatment to an effective amount of an aromatic amidine compound selected from the group consisting of 5-amidinoindole and 5-amidino-1-methylindole.

### Claim 2 (depends on 1)

The method of claim 1 wherein said amidine is administered in an effective amount ranging from about 1.0 to 10.0 M.

### Claim 3 (depends on 1, 2)

The method of claim 1 or 2 wherein said amidine is 5-amidino-1-methylindole.

### Claim 4 (depends on 1)

The method of claim 1 wherein the mode of administration is oral.

### Claim 5 (depends on 1)

The method of claim 1 wherein the host is a human.